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colesevelam

Bile Acid Sequestrant · Antihyperlipidemic

Bile Acid SequestrantAntihyperlipidemic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
5 major
SEVERE in our sources
PREGNANCY
B
FDA category + note
Top interactionssee all 10
  • BexaroteneSevereDatabaseDDInter
  • Mycophenolate MofetilSevereDatabaseDDInter
  • Mycophenolic AcidSevereDatabaseDDInter
  • TeriflunomideSevereDatabaseDDInter

Mechanism

Colesevelam is highly positively charged and binds negatively charged bile acids in the intestine, preventing their reabsorption and promoting excretion in stool. This depletes the bile acid pool, stimulating hepatic bile acid synthesis and increasing LDL receptor production, which enhances LDL-C clearance from plasma. This effect is partially offset by enhanced cholesterol synthesis.

Indications

HyperlipidemiaLowering LDL-C in patients with hypertriglyceridemiaTreatment of type 2 diabetes (as an adjunct to diet and exercise)Hypercholesterolemia

Dosing

Adult
Starting dose is either 3 tablets (0.625g each) taken twice daily with meals or all 6 tablets taken once daily with a meal. Maximum daily dose is 7 tablets (4.375 g).

Side effects

Common
Constipation (may be prevented by adequate daily water intake and psyllium)Less likely than colestipol to cause dyspepsia, bloating, and constipationConstipationDyspepsiaAbdominal painNausea

Pregnancy & lactation

Pregnancy

B

Drug interactions

Bexarotene
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Mycophenolate Mofetil
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Mycophenolic Acid
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Teriflunomide
Severe
Database

Drug interaction classified as: absorption, metabolism

Source: DDInter

Ursodeoxycholic Acid
Severe
Database

Decreased efficacy of ursodeoxycholic acid.

Administer ursodeoxycholic acid at least 2 hours before or 4-6 hours after colesevelam. Monitor for therapeutic effect.

Ethinyl Estradiol
Moderate
Textbook

Altered plasma levels and efficacy of ethinyl estradiol, potentially reducing contraceptive effect.

Source: G&G 14e · p1041

Fat Soluble Vitamins
Moderate
Textbook

Reduced absorption of fat-soluble vitamins (A, D, E, K).

Source: G&G 14e · p1041

Glyburide
Moderate
Textbook

Altered plasma levels and efficacy of glyburide, potentially affecting glycemic control.

Source: G&G 14e · p1041

L Thyroxine
Moderate
Textbook

Altered plasma levels and efficacy of L-thyroxine.

Source: G&G 14e · p1041

Verapamil
Moderate
Textbook

Reduced exposure and efficacy of sustained-release verapamil.

Prudence suggests patients take other medications 1 h before or 3 to 4 h after a dose of colesevelam.

Source: G&G 14e · p738

2 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Other Bile Acid Sequestrant drugs

Ask House about colesevelam

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team